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Heterocyclic amides as ROCK inhibitors

A technology of -OR21 and alkyl, applied in the direction of medical preparations containing active ingredients, digestive system, cardiovascular system diseases, etc., can solve problems such as leakage

Active Publication Date: 2013-01-16
PH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As for dermal administration, local injection and implantable medical devices, there is a serious risk of leakage into the systemic circulation

Method used

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  • Heterocyclic amides as ROCK inhibitors
  • Heterocyclic amides as ROCK inhibitors
  • Heterocyclic amides as ROCK inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0369] A. Physicochemical Properties of Compounds

[0370] A.1. Purity of compounds

[0371] Unless otherwise stated, the purity of compounds will be confirmed by liquid chromatography / mass spectrometry (LC / MS) as follows:

[0372] ·HPLC system: Waters2690 and Waters996 photodiode array detector; column: C18; gradient: solvent A (H 2 O / formic acid 26.5nM) 0%, to solvent B (CH 3 CN / formic acid 17nM) 80% within 3 minutes. Flow rate: 2.75ml / min.

[0373] · Mass Spectrometer: Micellar Platform LC. Ionization: electrospray (polarity: negative and positive)

[0374]A.2. Division of configuration:

[0375] The absolute configuration of the asymmetric center is assigned using the Cahn-Ingold-Prelog system, in which the four groups of asymmetric carbons will be ranked according to a set of sequence rules. For reference see Cahn; Ingold; Prelog Angew. Chem. Int. Ed. Eng / .1966, 5, 385-415.

[0376] A.3. Stereochemistry:

[0377] It is known to those skilled in the art that spec...

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Abstract

The present invention relates to new kinase inhibitors of formula (I), more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

Description

technical field [0001] The present invention relates to a novel kinase inhibitor, more specifically a ROCK inhibitor, a composition containing this inhibitor, especially a medicine, and the use of the inhibitor in the treatment and prevention of diseases. In particular, the present invention relates to a novel ROCK inhibitor, a composition comprising such an inhibitor, especially a medicament, and the use of the inhibitor in the treatment and prevention of diseases. Background technique [0002] Serine / threonine protein kinase ROCK consists of two isoforms ROCK I and ROCK II in the human body. ROCK I is encoded on chromosome 18, while ROCK II (also known as Rho kinase) is located on chromosome 12. Both have a molecular mass of about 160kD. The two (amino acid sequences) have 65% homology, and the homology of the kinase region is as high as 95%. Although their sequences are similar, their tissue distributions vary. The highest levels of ROCK I expression are observed in h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/75C07D239/42C07D471/04C07D401/12C07D405/12C07D409/12C07D493/04A61K31/437A61K31/4409A61K31/4433A61K31/443A61K31/4436A61K31/505A61P1/00A61P9/00
Inventor D・雷森O・戴非尔特N・卡瓦尔P・布罗姆S・波兰德
Owner PH PHARMA CO LTD
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